{"title":"用不同药物聚合物制备的静电纺丝纳米纤维增强普罗布考的溶解度和控释。","authors":"Saki Arakawa, Kouji Hara, Yoko Koide, Mayumi Yamada, Eriko Yamazoe, Takaaki Ito, Kohei Tahara","doi":"10.1080/10837450.2025.2562205","DOIUrl":null,"url":null,"abstract":"<p><p>We aimed to improve the water solubility and control the release of probucol using electrospinning technology. The effects of multiple polymer matrices and surfactants on the water solubility of probucol were evaluated. Probucol-loaded nanofibers were prepared using four polymers: polyvinylacetal diethylaminoacetate (AEA), methacrylic acid/ethyl acrylate (1/1) copolymer (Kollicoat MAE), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG, Soluplus), and polyvinylpyrrolidone (PVP). Each polymer exhibited different solubility characteristics, and optimal manufacturing conditions were determined. Probucol was in an amorphous state within the nanofibers. The pH-sensitive polymers, including AEA and MAE, enhanced probucol solubility, enabling controlled release in response to pH changes. Additionally, incorporating the surfactants, Tween 80 and Span 20, improved the wettability of Soluplus nanofibers, further enhancing probucol solubility. The addition of surfactants reduced the fiber diameter of the nanofibers, increased the initial dissolution rate, and approximately doubled the drug release rate after 24 h. These findings indicate that the choice of polymer matrix and surfactant is critical for improving solubility and controlling the release of drugs with poor water solubility in electrospun nanofiber solid dispersions. These results provide valuable insights for the development of nanofiber formulations.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1-15"},"PeriodicalIF":2.5000,"publicationDate":"2025-09-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Enhanced solubility and controlled release of probucol using electrospun nanofibers prepared with different pharmaceutical polymers.\",\"authors\":\"Saki Arakawa, Kouji Hara, Yoko Koide, Mayumi Yamada, Eriko Yamazoe, Takaaki Ito, Kohei Tahara\",\"doi\":\"10.1080/10837450.2025.2562205\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>We aimed to improve the water solubility and control the release of probucol using electrospinning technology. The effects of multiple polymer matrices and surfactants on the water solubility of probucol were evaluated. Probucol-loaded nanofibers were prepared using four polymers: polyvinylacetal diethylaminoacetate (AEA), methacrylic acid/ethyl acrylate (1/1) copolymer (Kollicoat MAE), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG, Soluplus), and polyvinylpyrrolidone (PVP). Each polymer exhibited different solubility characteristics, and optimal manufacturing conditions were determined. Probucol was in an amorphous state within the nanofibers. The pH-sensitive polymers, including AEA and MAE, enhanced probucol solubility, enabling controlled release in response to pH changes. Additionally, incorporating the surfactants, Tween 80 and Span 20, improved the wettability of Soluplus nanofibers, further enhancing probucol solubility. The addition of surfactants reduced the fiber diameter of the nanofibers, increased the initial dissolution rate, and approximately doubled the drug release rate after 24 h. These findings indicate that the choice of polymer matrix and surfactant is critical for improving solubility and controlling the release of drugs with poor water solubility in electrospun nanofiber solid dispersions. These results provide valuable insights for the development of nanofiber formulations.</p>\",\"PeriodicalId\":20004,\"journal\":{\"name\":\"Pharmaceutical Development and Technology\",\"volume\":\" \",\"pages\":\"1-15\"},\"PeriodicalIF\":2.5000,\"publicationDate\":\"2025-09-29\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Development and Technology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/10837450.2025.2562205\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Development and Technology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/10837450.2025.2562205","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Enhanced solubility and controlled release of probucol using electrospun nanofibers prepared with different pharmaceutical polymers.
We aimed to improve the water solubility and control the release of probucol using electrospinning technology. The effects of multiple polymer matrices and surfactants on the water solubility of probucol were evaluated. Probucol-loaded nanofibers were prepared using four polymers: polyvinylacetal diethylaminoacetate (AEA), methacrylic acid/ethyl acrylate (1/1) copolymer (Kollicoat MAE), polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PCL-PVAc-PEG, Soluplus), and polyvinylpyrrolidone (PVP). Each polymer exhibited different solubility characteristics, and optimal manufacturing conditions were determined. Probucol was in an amorphous state within the nanofibers. The pH-sensitive polymers, including AEA and MAE, enhanced probucol solubility, enabling controlled release in response to pH changes. Additionally, incorporating the surfactants, Tween 80 and Span 20, improved the wettability of Soluplus nanofibers, further enhancing probucol solubility. The addition of surfactants reduced the fiber diameter of the nanofibers, increased the initial dissolution rate, and approximately doubled the drug release rate after 24 h. These findings indicate that the choice of polymer matrix and surfactant is critical for improving solubility and controlling the release of drugs with poor water solubility in electrospun nanofiber solid dispersions. These results provide valuable insights for the development of nanofiber formulations.
期刊介绍:
Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology.
Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as:
-Preformulation and pharmaceutical formulation studies
-Pharmaceutical materials selection and characterization
-Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation
-QbD in the form a risk assessment and DoE driven approaches
-Design of dosage forms and drug delivery systems
-Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies
-Drug delivery systems research and quality improvement
-Pharmaceutical regulatory affairs
This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.